Invention Application
- Patent Title: INHIBITORS OF HUMAN EZH2, AND METHODS OF USE THEREOF
- Patent Title (中): 人类EZH2的抑制剂及其使用方法
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Application No.: US15132610Application Date: 2016-04-19
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Publication No.: US20170065600A1Publication Date: 2017-03-09
- Inventor: Kevin Wayne Kuntz , Sarah Kathleen Knutson , Timothy James Nelson Wigle , Robert A. Copeland , Victoria M. Richon , Margaret D. Scott , Christopher J. Sneeringer , Roy M. Pollock
- Applicant: EPIZYME, INC.
- Main IPC: A61K31/5377
- IPC: A61K31/5377 ; A61K31/444 ; A61K31/4545 ; A61K31/551 ; G01N33/50 ; A61K31/4439 ; A61K31/4427 ; A61K31/496 ; A61K31/497 ; A61K31/7076 ; A61K31/4412

Abstract:
The invention relates to inhibition of wild-type and certain mutant forms of human histone methyltransferase EZH2, the catalytic subunit of the PRC2 complex which catalyzes the mono- through tri-methylation of lysine 27 on histone H3 (H3-K27). In one embodiment the inhibition is selective for the mutant form of the EZH2, such that trimethylation of H3-K27, which is associated with certain cancers, is inhibited. The methods can be used to treat cancers including follicular lymphoma and diffuse large B-cell lymphoma (DLBCL). Also provided are methods for identifying small molecule selective inhibitors of the mutant forms of EZH2 and also methods for determining responsiveness to an EZH2 inhibitor in a subject.
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